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A novel structural class of potent inhibitors of NF-κB activation: structure–activity relationships and biological effects of 6-aminoquinazoline derivatives

…, Y Isobe, H Tomizawa, T Nagasaki, H Takahashi…

文献索引:Tobe, Masanori; Isobe, Yoshiaki; Tomizawa, Hideyuki; Nagasaki, Takahiro; Takahashi, Hirotada; Hayashi, Hideya Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 18 p. 3869 - 3878

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被引用次数: 64

摘要

In this study, we have investigated the roles of substituents on the terminal phenyl ring at the C (4)-position of the quinazoline core to complete the structure–activity relationships (SARs) of our NF-κB activation inhibitors. Among them, compound 12j afforded highly potent inhibitory activity toward NF-κB transcriptional activation with IC50 value of 2nM, along with an excellent in vivo efficacy by reducing the edema formation seen in carrageenin- ...

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